2. Academic Validation
  3. Therapeutic potential of IKK-β inhibitors from natural phenolics for inflammation in cardiovascular diseases

Therapeutic potential of IKK-β inhibitors from natural phenolics for inflammation in cardiovascular diseases

  • Inflammopharmacology. 2020 Feb;28(1):19-37. doi: 10.1007/s10787-019-00680-8.
Peng Zhou 1 2 3,  Fang Hua 4 5,  Xiang Wang 6 7 8,  Jin-Ling Huang 9 10 11
Affiliations

Affiliations

  • 1 School of Integrated Chinese and Western Medicine, Anhui University of Chinese Medicine, Hefei, 230012, People's Republic of China. zp0108@126.com.
  • 2 Institute of Integrated Chinese and Western Medicine, Anhui Academy of Chinese Medicine, Hefei, 230012, People's Republic of China. zp0108@126.com.
  • 3 Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, 230012, People's Republic of China. zp0108@126.com.
  • 4 Pharmacy School, Anhui Xinhua University, Hefei, 230088, People's Republic of China.
  • 5 Natural Products Laboratory, International Joint Lab of Tea Chemistry and Health Effects, State Key Laboratory of Tea Plant Biology and Utilization, Anhui Agricultural University, Hefei, 230036, People's Republic of China.
  • 6 School of Integrated Chinese and Western Medicine, Anhui University of Chinese Medicine, Hefei, 230012, People's Republic of China.
  • 7 Institute of Integrated Chinese and Western Medicine, Anhui Academy of Chinese Medicine, Hefei, 230012, People's Republic of China.
  • 8 Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, 230012, People's Republic of China.
  • 9 School of Integrated Chinese and Western Medicine, Anhui University of Chinese Medicine, Hefei, 230012, People's Republic of China. jinling6181@126.com.
  • 10 Institute of Integrated Chinese and Western Medicine, Anhui Academy of Chinese Medicine, Hefei, 230012, People's Republic of China. jinling6181@126.com.
  • 11 Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, 230012, People's Republic of China. jinling6181@126.com.
PMID: 31894515 DOI: 10.1007/s10787-019-00680-8
Abstract

Cardiovascular Disease (CVDs) is a chronic disease with the highest morbidity and mortality in the world. Previous studies have suggested that preventing inflammation serves an efficient role in protection against cardiovascular diseases. Modulation of IKK-β activity can be used to treat and control CVDs associated with chronic inflammation, which targets the phosphorylation of IκB following the release of the RelA complex, and then translocates to the nucleus, eventually triggering the transcription of several genes that induce chemokines, cytokines, and adhesion molecules. Most importantly, the IκB kinase (IKK) complex is involved in transcriptional activation by phosphorylating the inhibitory molecule IkBα, enabling activation of NF-κB. Phenolic compounds possess cardioprotective potential that may be related to modulating inflammatory responses involved in CVDs. The SystemsDock analysis was used to explore whether 38 active compounds inhibit IKK-β activity based on literature. Docking results showed that the top docking score of three chemical compounds were icariin, salvianolic acid B, and plantainoside D in all compounds. Icariin, salvianolic acid B, and plantainoside D are the most promising IKKβ inhibitors. These phytochemicals could be helpful to find the lead compounds on designing and developing novel cardioprotective agents.

Keywords

Cardiovascular diseases; Ikk-β inhibitor; Molecular docking; NF-κb; Phenolic compounds.

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